Background and purpose: The phytocannabinoid, Δ 9- tetrahydrocannabivarin (THCV), can block cannabinoid CB 1 receptors. This investigation explored its ability to activate CB 2 receptors, there being evidence that combined CB 2 activation/CB 1 blockade would ameliorate certain disorders. Experimental approach: We tested the ability of THCV to activate CB 2 receptors by determining whether: (i) it inhibited forskolin-stimulated cyclic AMP production by Chinese hamster ovary (CHO) cells transfected with human CB 2 (hCB 2) receptors; (ii) it stimulated [ 35S]GTPγS binding to hCB 2 CHO cell and mouse spleen membranes; (iii) it attenuated signs of inflammation/hyperalgesia induced in mouse hind paws by intraplantar injection of carrageenan or formalin; and (iv) any such anti-inflammatory or anti-hyperalgesic effects were blocked by a CB 1 or CB 2 receptor antagonist. Key results: THCV inhibited cyclic AMP production by hCB 2 CHO cells (EC 50 = 38 nM), but not by hCB 1 or untransfected CHO cells or by hCB 2 CHO cells pre-incubated with pertussis toxin (100 ng·mL -1) and stimulated [ 35S]GTPγS binding to hCB 2 CHO and mouse spleen membranes. THCV (0.3 or 1 mg·kg -1 i.p.) decreased carrageenan-induced oedema in a manner that seemed to be CB 2 receptor-mediated and suppressed carrageenan-induced hyperalgesia. THCV (i.p.) also decreased pain behaviour in phase 2 of the formalin test at 1 mg·kg -1, and in both phases of this test at 5 mg·kg -1; these effects of THCV appeared to be CB 1 and CB 2 receptor mediated. Conclusions and implications: THCV can activate CB 2 receptors in vitro and decrease signs of inflammation and inflammatory pain in mice partly via CB 1 and/or CB 2 receptor activation. © 2010 The British Pharmacological Society All rights reserved.

Bolognini, D., Costa, B., Maione, S., Comelli, F., Marini, P., Di Marzo, V., et al. (2010). The plant cannabinoid Δ 9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice. BRITISH JOURNAL OF PHARMACOLOGY, 160(3), 677-687 [10.1111/j.1476-5381.2010.00756.x].

The plant cannabinoid Δ 9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice

COSTA, BARBARA SIMONA;COMELLI, FRANCESCA;
2010

Abstract

Background and purpose: The phytocannabinoid, Δ 9- tetrahydrocannabivarin (THCV), can block cannabinoid CB 1 receptors. This investigation explored its ability to activate CB 2 receptors, there being evidence that combined CB 2 activation/CB 1 blockade would ameliorate certain disorders. Experimental approach: We tested the ability of THCV to activate CB 2 receptors by determining whether: (i) it inhibited forskolin-stimulated cyclic AMP production by Chinese hamster ovary (CHO) cells transfected with human CB 2 (hCB 2) receptors; (ii) it stimulated [ 35S]GTPγS binding to hCB 2 CHO cell and mouse spleen membranes; (iii) it attenuated signs of inflammation/hyperalgesia induced in mouse hind paws by intraplantar injection of carrageenan or formalin; and (iv) any such anti-inflammatory or anti-hyperalgesic effects were blocked by a CB 1 or CB 2 receptor antagonist. Key results: THCV inhibited cyclic AMP production by hCB 2 CHO cells (EC 50 = 38 nM), but not by hCB 1 or untransfected CHO cells or by hCB 2 CHO cells pre-incubated with pertussis toxin (100 ng·mL -1) and stimulated [ 35S]GTPγS binding to hCB 2 CHO and mouse spleen membranes. THCV (0.3 or 1 mg·kg -1 i.p.) decreased carrageenan-induced oedema in a manner that seemed to be CB 2 receptor-mediated and suppressed carrageenan-induced hyperalgesia. THCV (i.p.) also decreased pain behaviour in phase 2 of the formalin test at 1 mg·kg -1, and in both phases of this test at 5 mg·kg -1; these effects of THCV appeared to be CB 1 and CB 2 receptor mediated. Conclusions and implications: THCV can activate CB 2 receptors in vitro and decrease signs of inflammation and inflammatory pain in mice partly via CB 1 and/or CB 2 receptor activation. © 2010 The British Pharmacological Society All rights reserved.
Articolo in rivista - Articolo scientifico
Scientifica
Δ ; 9; -Tetrahydrocannabivarin; Carrageenan; CB ; 1; receptor; CB ; 2; receptor; CP55940; Formalin; Inflammation; Pain; Pertussis toxin;
English
Green Open Access
Bolognini, D., Costa, B., Maione, S., Comelli, F., Marini, P., Di Marzo, V., et al. (2010). The plant cannabinoid Δ 9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice. BRITISH JOURNAL OF PHARMACOLOGY, 160(3), 677-687 [10.1111/j.1476-5381.2010.00756.x].
Bolognini, D; Costa, B; Maione, S; Comelli, F; Marini, P; Di Marzo, V; Parolaro, D; Ross, R; Gauson, L; Cascio, M; Pertwee, R
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10281/15708
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